olvanil [Ligand Id: 2488] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL76903 (TCMDC-124289, NE-19550, Olvanil)
  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • GPR119 in Human [GtoPdb: 126] [UniProtKB: Q8TDV5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
ChEMBL Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 5.77 pIC50 1700 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
ChEMBL Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry B 6.8 pIC50 160 nM IC50 J Med Chem (2018) 61: 8255-8281 [PMID:30176215]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
GtoPdb - - 7.7 pEC50 19.9 nM EC50 Eur J Pharmacol (2001) 417: 51-8 [PMID:11301059]
ChEMBL Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpressing the human VR1 F 9.3 pEC50 0.5 nM EC50 J. Med. Chem. (2002) 45: 3739-3745 [PMID:12166946]
TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3]
GtoPdb - - 8.4 pEC50 - - - Neurosci Lett (2004) 370: 55-60 [PMID:15489017]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells B 6.85 pKi 142 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 5227-5231 [PMID:22796184]
ChEMBL Agonist activity at rat TRPV1 expressed in CHO cells assessed as calcium uptake F 6.69 pEC50 202 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 5227-5231 [PMID:22796184]
GtoPdb - - 8.1 pEC50 - - - Br J Pharmacol (2000) 130: 916-22 [PMID:10864900]
GPR119 in Human [GtoPdb: 126] [UniProtKB: Q8TDV5]
GtoPdb - - 5.1 pEC50 - - - Mol Endocrinol (2010) 24: 161-70 [PMID:19901198]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]